Central Cholinergic Agents. IV. Synthesis and Acetylcholinesterase Inhibitory Activities of ω-[N-Ethyl-N-(phenylmethyl)amino]-1-phenyl-1-alkanones and Their Analogues with Partical Conformational Restriction

概要

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Inhibitors of acetylcholinesterase (AChE) have been designed based on a working hypothesis of the enzyme's active site. These compounds were tested for their inhibitory activities on AChE and ω-[N-ethyl-N-(phenylmethyl)amino]-1-phenyl-1-alkanones (3) were found to be potent inhibitors. Various analogues of 3 were prepared to study the effect on AChE inhibition of partial restriction of conformation. Compounds with potent AChE inhibition were further evaluated in terms of central selectivity : the ratio of central action (ameliorationg effect on scopolamine-induced memory impairment using a T-maze alternation task) to peripheral action.
公益社団法人日本薬学会の論文
1993-03-15